Resources for Human Health from the Plant Kingdom: The Potential Role of the Flavonoid Apigenin in Cancer Counteraction

Abstract

Apigenin is one of the most widespread flavonoids in the plant kingdom. For centuries, apigenin-containing plant preparations have been used in traditional medicines to treat diseases that have an inflammatory and/or degenerative component. In the 1980s, apigenin was proposed to interfere with the process of carcinogenesis. Since then, more and more evidence has demonstrated its anticancer efficacy, both in vitro and in vivo. Apigenin has been shown to target signaling pathways involved in the development and progression of cancer, such as PI3K/Akt/mTOR, MAPK/ERK, JAK/STAT, NF-κB, and Wnt/β-catenin pathways, and to modulate different hallmarks of cancer, such as cell proliferation, metastasis, apoptosis, invasion, and cell migration. Furthermore, apigenin modulates PD1/PD-L1 expression in cancer/T killer cells and regulates the percentage of T killer and T regulatory cells. Recently, apigenin has been studied for its synergic and additive effects when combined with chemotherapy, minimizing the side effects. Unfortunately, its low bioavailability and high permeability limit its therapeutic applications. Based on micro- and nanoformulations that enhance the physical stability and drug-loading capacity of apigenin and increase the bioavailability of apigenin, novel drug-delivery systems have been investigated to improve its solubility.

Assessment of the biological activity of Marrubium friwaldskyanum Boiss. (Lamiaceae)

“…Luteoloside was specifically detected in the flowers of M. friwaldskyanum [ 19 ]. This flavonoid possess diverse biological activities including strong antitumor potential [ 32 ].The better properties of the extract obtained from flowers could be also attributed to the reported higher levels of chlorogenic acid, apigenin, kaempherol and quercetin – compounds that are well known for their antitumor properties [ [33] , [34] , [35] , [36] ]. Specifically abundant in M. friwaldskyanum leaves were isorhamnetin–3- O -rutinoside and isorhamnetin–3- O -glucoside [ 19 ].…”

Biliary tract dysfunctions: Possibilities of combined drugs of plant origin as advantage therapy

“…Апигенин способен снижать поглощение глюкозы раковыми клетками, ингибировать ремоделирование внеклеточного матрикса, ингибировать молекулы клеточной адгезии, которые участвуют в прогрессировании рака, и противодействовать сигнальным путям хемокинов, которые направляют метастазирование в другие места. В итальянском обзоре [52], опубликованном в декабре 2023 г., отмечается, что апигенин воздействует на сигнальные пути, участвующие в развитии и прогрессировании рака, такие как PI3K/Akt/mTOR, MAPK/ERK, JAK/STAT, NF-κB и Wnt/β-катенин, а также модулирует различные признаки рака, такие как пролиферация клеток, метастазирование, апоптоз, инвазия и миграция клеток. Кроме того, апигенин модулирует экспрессию PD1/PD-L1 в раковых/Т-киллерных клетках и регулирует процентное содержание Т-киллеров и Т-регуляторных клеток.…”

“…Кроме того, апигенин модулирует экспрессию PD1/PD-L1 в раковых/Т-киллерных клетках и регулирует процентное содержание Т-киллеров и Т-регуляторных клеток. Апигенин рассматривается в аспекте его синергического и аддитивного действия в сочетании с химиотерапией, сводящего к минимуму побочные эффекты [52].…”

Apigenin: A Bioflavonoid with a Promising Role in Disease Prevention and Treatment

“…24 [3,4]. It has three hydroxyl groups, with the first as well as second in the C5 and C7 positions, and the third at C4 ′ of the B ring [5].…”

“…Apigenin (4′,5,7-trihydroxyflavone) ( Figure 1 ) is a flavonoid present in fruits as well as vegetables, belonging to the flavone class that is the aglycone of several naturally occurring glycosides; its melting point is 347.5 °C, its chemical formula is C 15 H 10 O 5 , and its molecular weight is 270.24 [ 3 , 4 ]. It has three hydroxyl groups, with the first as well as second in the C5 and C7 positions, and the third at C4′ of the B ring [ 5 ].…”